Synthesis and structure–activity analysis of new phosphonium salts with potent activity against African trypanosomes

…, HP de Koning, A Chana, C Dardonville

文献索引：Taladriz, Andrea; Healy, Alan; Flores Perez, Eddysson J.; Herrero Garcia, Vanessa; Rios Martinez, Carlos; Alkhaldi, Abdulsalam A. M.; Eze, Anthonius A.; Kaiser, Marcel; De Koning, Harry P.; Chana, Antonio; Dardonville, Christophe Journal of Medicinal Chemistry, 2012 , vol. 55, # 6 p. 2606 - 2622

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被引用次数: 21

摘要

A series of 73 bisphosphonium salts and 10 monophosphonium salt derivatives were synthesized and tested in vitro against several wild type and resistant lines of Trypanosoma brucei (T. b. rhodesiense STIB900, T. b. brucei strain 427, Tb AT1-KO, and Tb B48). More than half of the compounds tested showed a submicromolar EC50 against these parasites. The compounds did not display any cross-resistance to existing diamidine therapies, such ...